| CAS NO: | 1191951-57-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 409.61 |
|---|---|
| Formula | C20H31N3O2S2 |
| CAS No. | 1191951-57-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 82 mg/mL (200.2 mM) |
| Water: <1 mg/mL | |
| Ethanol: 60 mg/mL (146.5 mM) | |
| Solubility (In vivo) | 5% DMSO+95% Corn oil: 5mg/mL |
| Other info | Synonym: PHT427; PHT-427; PHT 427. Chemical Name: 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide InChi Key: BYWWNRBKPCPJMG-UHFFFAOYSA-N InChi Code: InChI=1S/C20H31N3O2S2/c1-2-3-4-5-6-7-8-9-10-11-12-18-13-15-19(16-14-18)27(24,25)23-20-22-21-17-26-20/h13-17H,2-12H2,1H3,(H,22,23) SMILES Code: O=S(C1=CC=C(CCCCCCCCCCCC)C=C1)(NC2=NN=CS2)=O |
In Vitro | Kinase Assay: All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less.
Cell Assay: PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427 significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM, which shows that PHT-427 could inhibit both Akt and PDPK1. PHT-427 also inhibits translocation of the Akt and PDPK1 PH domains in plasma membrane. PHT-427 induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells with IC50 of 65 μM. |
In Vivo | PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7 breast and A-549 NSCL cancer xenografts. PHT-427 gives up to an 80% inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg. |
Animal model | BxPC-3, Panc-1, MiaPaCa-2, PC-3, SKOV-3, A-549 or MCF-7 cells are injected subcutaneously into the flanks of female scid mice. |
Formulation & Dosage | Formulated in 40 to 50 mg/mL in sesame seed oil; 125-250 mg/kg; oral gavage |
References | [1] Meuillet EJ, et al. Mol Cancer Ther, 2010, 9(3), 706-717.; [2] Moses SA, et al. Cancer Res, 2009, 69(12), 5073-5081. |
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